Cabergoline, sold under the brand name Dostinex among others, is a dopaminergic medication used in the treatment of high prolactin levels, prolactinomas, Parkinson's disease, and for other indications. It is taken by mouth.
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Cabergoline works mainly by activating dopamine receptors in the brain, particularly a type called D2 receptors. This action suppresses the release of prolactin, a hormone made by the pituitary gland. In Australia, it's approved for conditions where prolactin levels are abnormally high, for Parkinson disease, and to prevent lactation when breastfeeding isn't planned or medically advisable.
The medication also interacts with several other receptor types in the brain and body—including other dopamine receptors, serotonin receptors, and adrenergic receptors—sometimes activating them and sometimes blocking them. One of these interactions, with a serotonin receptor subtype called 5-HT2B, has been linked to heart valve problems in some people taking the drug. This doesn't mean everyone who takes cabergoline will develop valve issues, but it's a known risk your family member's doctor will monitor.
Cabergoline stays in the body for a long time after each dose—its half-life is estimated at 63 to 69 hours. That means it takes roughly three days for half of a single dose to clear, which is why it's usually given once or twice a week rather than daily. The long duration also means side effects, if they occur, may persist for several days after taking a dose.
Pathological hyperprolactinaemia Clinical criteria: The condition must be stable for the prescriber to consider the listed maximum quantity of this medicine suitable for this patient, AND Patient must be one in whom surgery is not indicated.
Parkinson disease Clinical criteria: The condition must be stable for the prescriber to consider the listed maximum quantity of this medicine suitable for this patient. Treatment criteria: Must be treated by a health practitioner who is any of: (i) a medical practitioner, (ii) an authorised PBS prescriber who is not a medical practitioner, but who is: (a) sharing care of the patient with at least one medical practitioner; (b) intending to share care of the patient with a medical practitioner.
“Cabergoline is a long-acting dopamine D2 receptor agonist. In-vitro rat studies show a direct inhibitory effect of cabergoline on the prolactin secretion in the lactotroph cells of the pituitary gland and cabergoline decreases serum prolactin levels in reserpinized rats.[citation needed] Although cabergoline is commonly described principally as a D2 receptor agonist, it also possesses significant affinity for the dopamine D3, and D4, serotonin 5-HT1A, 5-HT2A, 5-HT2B, and 5-HT2C, and α2-adrenergic receptors, as well as moderate/low affinity for the dopamine D1, serotonin 5-HT7, and α1-adrenergic receptors. Cabergoline functions as a partial or full agonist at all of these receptors except for the 5-HT7, α1-adrenergic, and α2-adrenergic receptors, where it acts as an antagonist. Cabergoline has been associated with cardiac valvulopathy due to activation of 5-HT2B receptors.”
“63–69 hours (estimated)”
Working under the parallel aged-care framework? Aged-care equivalent →
Prevention of the onset of lactation Clinical criteria: The treatment must occur in the puerperium, AND The treatment must be for medical reasons.